Adenosine receptor subtype selectivity of antagonists
| Antagonist | KI (nM) | |||
|---|---|---|---|---|
| A1 | A2A | A2B | A3 | |
| I-ABOPX | 70 ± 3 | 95 ± 15 | 30 ± 2 | 15 ± 2 |
| ZM214385 | 536 ± 63 | 1.4 ± 0.6 | 31 ± 1.0 | 269 ± 91 |
| CPX | 2.5 ± 0.1 | 156 ± 73 | 56 ± 8 | 509 ± 109 |
| Theophylline | 6,200 ± 1,500 | 4,200 ± 240 | 9,200 ± 750 | 52,300 ± 16,000 |
| Enprofylline | 44,000 ± 11,000 | 32,000 ± 7,800 | 6,300 ± 1,800 | 158,000 ± 70,000 |
KI values to inhibit radioligand binding to recombinant human adenosine receptors were measured in side-by-side assays on the same day using membranes derived from transfected HEK 293 cells and various radioligands as described in Experimental Procedures. Data are the means ± S.E. of triplicate experiments.